枳实与枳壳功效差异的物质基础研究

Aurantii Fructus Immaturus (AFI)(Zhishi) and Aurantii Fructus (AF)(Zhiqiao) are 2 famous-region drug of Jiangxi province. They are mainly from Citrus aurantium L and their cultivated varieties of dry young fruitlets (AFI ) or immature fruits (AF). They belong to rue family plant. Both of them are commonly used in clinical traditional Chinese medicine. The functions of AFI have the broken gas and removing food retention, phlegm resolving ruffian; AF regulating the flow of vital energy and removing obstruction toit and wide, modulating the flow of qi and removing tumescence. At present, it is neither reported in the literature on the differences of effective ingredients between AFI and AF nor expounded on the mechanism of action of AFI' "broken gas" and regulating the flow of "Qi" of AF. .Previous studies have testified that AFI and AF contain the same types of components, but the quantity of component is different. AFI and AF efficacy differences in clinical traditional Chinese medicine should be embodied in their respective active substance group according to a certain amount of combination ways. .This reseach project in Chinese medicine clinical medicine as the instruction, using the already established active component content determination method, combining modern pharmacological experiments, from the active substance group through multiple targets, multiple pathways play a role through integration, developing AFI and AF respective active substance group compatibility rule study, so as to reveal the efficiency variance material foundation betwen AFI and AF, and their efficacy differences in essence, for the establishment of AFI and AF objective evaluation of the quality standard and providing a scientific basis for traditional Chinese medicine clinical medication.

枳实、枳壳主要来源为芸香科植物酸橙（Citrus aurantium L．）及其栽培变种的干燥幼果(枳实)或未成熟果实(枳壳)，是中医临床常用中药。枳实功能破气消积，化痰散痞；枳壳理气宽中，行滞消胀。目前既没有文献报道枳实与枳壳功效差异的物质基础，也没有文献阐述枳实的"破气"和枳壳"理气"的作用机制。前期研究结果表明枳实与枳壳所含绝大多数成分种类相同，只是所含成分有量的不同，其功效差异应该是体现在各自的活性物质群按一定量的配伍组合方面。本课题以中医临床用药为指导，采用已经建立的活性成分含量测定方法，结合现代药理实验，从活性物质群通过多靶点、多途径经整合发挥作用方面，开展枳实与枳壳各自的活性物质群的配伍组合规律研究，以达到揭示枳实与枳壳功效差异的物质基础，阐述枳实（壳）功效差异性实质，为建立枳实与枳壳客观评价的质量标准和中医临床用药提供科学依据。

枳实、枳壳主要来源为芸香科植物酸橙（Citrus aurantium L．）及其栽培变种的干燥幼果(枳实)或未成熟果实(枳壳)，均是中医临床常用中药。枳实功能破气消积，化痰散痞；枳壳理气宽中，行滞消胀。目前既没有文献报道枳实与枳壳功效差异的物质基础，也没有文献阐述枳实的“破气”和枳壳“理气”的作用机制。课题采用HPLC法测定枳实和枳壳所含的主要化学成分，比较两者之间所含成分的种类和含量之间的差异；对其所含单体成分分别进行动物离体组织和整体动物实验，并采用单体化合物进行组合模拟枳实水煎液进行药效试验，找寻枳实和枳壳主要活性成分，结果表明枳实和枳壳含有的一个活性物质群，主要是由柚皮苷、新橙皮苷、芸香柚皮苷、橙皮苷、川陈皮素、辛弗林和葡萄内酯等组成，所含活性成分对实验动物胃肠作用机制各异，证明活性物质群是通过多靶点、多途径经整合发挥枳壳的“理气”和枳实的“破气”的功效的，.枳实与枳壳两者功效差异的物质基础主要体现在成分种类和含量配比上，具体为：.① 枳壳的主要药效物质为：柚皮苷和新橙皮苷；.② 枳实的主要药效物质为：柚皮苷、新橙皮苷和辛弗林；.③ 枳实的主要药效物质柚皮苷和新橙皮苷的含量高于枳壳；.④ 枳壳与枳实的最终主要药效物质基础推测是柚皮苷和新橙皮苷及芸香柚皮苷和橙皮苷的代谢产物，即是：苷元（柚皮素和橙皮素）。.枳实与枳壳两者促进胃肠动力的作用机制可能通过升高血清中GAS、血浆中ACh、MTL、SP含量和抑制VIP的分泌来促进胃肠运动。.课题通过对枳实与枳壳各自的活性物质群的配伍组合规律研究，达到揭示枳实与枳壳功效差异的物质基础的目的，阐述枳实、枳壳功效差异性实质，可为建立枳实与枳壳客观评价的质量标准和中医临床用药提供科学依据。